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HIV Protease (Wild Type L63P) recombinant, expressed in E. coli Catalog Number H1415 Storage Temperature –70 °C CAS RN 144114-21-6 EC 3.4.23.16 Synonyms: HIV-1 Protease; Retropepsin; HIV PR Product Description HIV (HIV-1) protease is an aspartic protease with a significant role in HIV replication. It cleaves the two HIV polyprotein chains, activating the mature protein components to produce new viruses. This action makes the HIV protease a major drug target for treating HIV. The HIV-1 protease prefers cleavage between an aromatic residue (Tyr or Phe) and a Pro residue. Alternatively, HIV-1 protease prefers to cleave between hydrophobic residues.2 This product has been engineered to include the most commonly occurring polymorphism (L63P) as measured in the treated HIV population. This polymorphism is accessory in that it normally occurs with other key point mutations that add to the drug resistance profile of the protease. Practically, the L63P mutation can be considered to be the newest “wild type” sequence, as the virus has mutated since its discovery due to pressure from current protease inhibitor based therapy. This product is especially useful for high throughput screening of drug compound libraries and for general kinetic assays.2 The product is supplied as a solution in 0.5 M sodium acetate, pH 4.7, with 50 mM Tris-HCl, 1 M NaCl, 1 mM EDTA, 5 mM DTT, and 15% glycerol. HIV-1 protease can be inhibited with aspartic acid type protease inhibitors, such as acetyl-pepstatin, as well as commercially available HIV-1 protease inhibitors that are currently being used as drugs.2 Activity: HIV protease activity has been determined with the fluorescent substrate: Abz-Ala-Arg-Val-NleTyr(NO2)-Glu-Ala-Nle-NH2. HIV protease is a homodimer, with each monomer containing 99 amino acids.1 Each monomer subunit contains 1 α-helix and 2 anti-parallel β sheets. Unit definition: One unit of HIV protease will cleave 1 picomole per minute of the substrate Abz-Ala-ArgVal-Nle-Tyr(NO2)-Glu-Ala-Nle-NH2 at pH 5.5 and 37 °C. 2 Molecular mass: 10.8 kDa Isoelectric point:2 9.1 Optimal pH range:2 4.7–5.5 Precautions and Disclaimer This product is for R&D use only, not for drug, household, or other uses. Please consult the Material Safety Data Sheet for information regarding hazards and safe handling practices. Storage/Stability Store the product at –70 °C. It remains active at room temperature for 1 hour.2 References 1. Davies, D. R., The Structure and Function of the Aspartic Proteinases. Annual Review of Biophysics and Biophysical Chemistry, 19, 189-215 (1990). 2. Supplier Data CS,MAM 09/08-1 Sigma brand products are sold through Sigma-Aldrich, Inc. Sigma-Aldrich, Inc. warrants that its products conform to the information contained in this and other Sigma-Aldrich publications. Purchaser must determine the suitability of the product(s) for their particular use. Additional terms and conditions may apply. Please see reverse side of the invoice or packing slip.